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Saturated Fatty Acid-Based In Situ Forming Matrices for Localized Antimicrobial Delivery

Overview
Journal Pharmaceutics
Publisher MDPI
Date 2020 Aug 29
PMID 32854439
Citations 11
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Abstract

In recent years, the world has faced the issue of antibiotic resistance. Methicillin-resistant (MRSA) is a significant problem in various treatments and control of infections. Biocompatible materials with saturated fatty acids of different chain lengths (C-C) were studied as matrix formers of localized injectable vancomycin HCl (VCM)-loaded antisolvent-induced in situ forming matrices. The series of fatty acid-based in situ forming matrices showed a low viscosity (5.47-13.97 cPs) and pH value in the range of 5.16-6.78, with high injectability through a 27-G needle (1.55-3.12 N). The preparations exhibited low tolerance to high concentrations of KHPO solution (1.88-5.42% ) and depicted an electrical potential change during phase transformation. Their phase transition and matrix formation at the microscopic and macroscopic levels depended on the chain length of fatty acids and solvent characteristics. The VCM release pattern depended on the nucleation/crystallization and solvent exchange behaviors of the delivery system. The 35% of C-C fatty acid-based in situ forming matrix prolonged the VCM release over seven days in which C, C, C -based formulation reached 56, 84, and 85% cumulative drug release at 7 day. The release data fitted well with Higuchi's model. The developed formulations presented efficient antimicrobial activities against standard , MRSA, , and . Hence, VCM-loaded antisolvent-induced fatty acid-based in situ forming matrix is a potential local delivery system for the treatment of local Gram-positive infection sites, such as joints, eyes, dermis of surgery sites, etc., in the future.

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